BPN14770 CAS 1606974-33-7

BPN14770 CAS 1606974-33-7 is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D), with IC50 values ​​of 7.8 nM for PDE4D7 and 7.4 nM for PDE4D3. Zatolmilast is an investigational candidate in a pivotal clinical phase globally, specifically designed to address Fragile X syndrome, a rare neurodevelopmental disorder.

As the world's first highly selective allosteric modulator targeting PDE4D, its core function lies in precisely regulating the intracellular cyclic adenosine monophosphate (cAMP) signaling pathway. By specifically inhibiting the two isoforms PDE4D3 and PDE4D7, it effectively increases intracellular cAMP concentration, thereby activating the downstream CREB signaling pathway, promoting the synthesis and release of brain-derived neurotrophic factor (BDNF), repairing damaged synaptic connections at the molecular level, enhancing synaptic plasticity in the brain, and systematically improving cognitive, language, and neurological functions. Fragile X syndrome, as the leading cause of inherited intellectual disability and autism spectrum disorder, has long lacked targeted intervention programs. Zatolmilast, with its unique mechanism of action, is expected to fill this gap.